Clinical Pharmacokinetics

, Volume 43, Issue 12, pp 823–832 | Cite as

Effect of Mycophenolate Mofetil on the Pharmacokinetics of Antiretroviral Drugs and on Intracellular Nucleoside Triphosphate Pools

  • Sanjay U. C. Sankatsing
  • Patrick G. Hoggard
  • Alwin D. R. Huitema
  • Rolf W. Sparidans
  • Stephen Kewn
  • Kristel M. L. Crommentuyn
  • Joep M. A. Lange
  • Jos H. Beijnen
  • David J. Back
  • Jan M. Prins
Original Research Article



To study the effect of mycophenolate mofetil therapy on the pharmacokinetic parameters of a number of antiretroviral drugs, on intracellular pools of deoxycytidine triphosphate (dCTP) and deoxyguanosine triphosphate (dGTP), and on intracellular concentrations of the triphosphate of lamivudine (3TCTP).


Randomised pharmacokinetic study.


Nineteen HIV-1-infected patients.


Antiretroviral-naive men starting treatment with didanosine 400mg once daily, lamivudine 150mg twice daily, abacavir 300mg twice daily, indinavir 800mg twice daily, ritonavir 100mg twice daily and nevirapine 200mg twice daily were randomised to a group with or without mycophenolate mofetil 500mg twice daily. After 8 weeks of therapy, the plasma pharmacokinetic profiles of mycophenolic acid (the active metabolite of mycophenolate mofetil), abacavir, indinavir and nevirapine, and triphosphate concentrations (dCTP, dGTP and 3TCTP) in peripheral blood mononuclear cells, were determined.


Nine of the 19 patients received mycophenolate mofetil. There was no difference in plasma clearance of indinavir or abacavir between the two groups. The clearance of nevirapine was higher in patients using mycophenolate mofetil (p = 0.04). In 12 patients, of whom five also received mycophenolate mofetil, intracellular triphosphates were measured. There was no significant difference in intracellular dCTP, dGTP or 3TCTP concentrations between the two groups. Conclusion: In this small cohort of patients, mycophenolate mofetil therapy reduced the plasma concentration of nevirapine but had no effect on plasma concentrations of indinavir and abacavir. There were no consistent effects of mycophenolic acid on the intracellular concentrations of dCTP, dGTP or 3TCTP.


Nevirapine Mycophenolate Mofetil Indinavir Abacavir Mycophenolic Acid 
These keywords were added by machine and not by the authors. This process is experimental and the keywords may be updated as the learning algorithm improves.



We thank Marijke Roos, Sanquin Research and Landsteiner Laboratory, University of Amsterdam, Amsterdam, The Netherlands, for measuring lymphocyte proliferation. This study was financially supported by a private foundation that wishes not to be named.

Part of this study was presented at the 10th Conference on Retroviruses and Opportunistic Infections, Boston, MA, USA in February 2003.

The authors have no conflicts of interest that are directly relevant to the content of this study.


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Copyright information

© Adis Data Information BV 2004

Authors and Affiliations

  • Sanjay U. C. Sankatsing
    • 1
    • 2
  • Patrick G. Hoggard
    • 3
  • Alwin D. R. Huitema
    • 4
  • Rolf W. Sparidans
    • 5
  • Stephen Kewn
    • 3
  • Kristel M. L. Crommentuyn
    • 4
  • Joep M. A. Lange
    • 1
    • 2
  • Jos H. Beijnen
    • 4
    • 5
  • David J. Back
    • 3
  • Jan M. Prins
    • 2
  1. 1.International Antiviral Therapy Evaluation CenterAmsterdamThe Netherlands
  2. 2.Department of Internal Medicine, Division of Infectious Diseases, Tropical Medicine and AIDS, Academic Medical CenterUniversity of AmsterdamAmsterdamThe Netherlands
  3. 3.Department of Pharmacology and TherapeuticsUniversity of LiverpoolLiverpoolUK
  4. 4.Department of Pharmacy and PharmacologySlotervaart HospitalAmsterdamThe Netherlands
  5. 5.Department of Drug ToxicologyUtrecht UniversityUtrechtThe Netherlands

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